Authors
Katharina Elisabeth Grafinger, Marthe M Vandeputte, Annelies Cannaert, Adam Ametovski, Eric Sparkes, Elizabeth Cairns, Patrick Osamu Juchli, Belal Haschimi, Benedikt Pulver, Samuel D Banister, Christophe P Stove, Volker Auwärter
Publication date
2021/7
Journal
Drug testing and analysis
Volume
13
Issue
7
Pages
1412-1429
Description
The present work is the last of a three‐part study investigating a panel of 30 systematically designed synthetic cannabinoid receptor agonists (SCRAs) including features such as the 4‐pentenyl tail and varying head groups including amides and esters of l‐valine (MMB, AB), ltert‐leucine (ADB), and l‐phenylalanine (APP), as well as adamantyl (A) and cumyl moieties (CUMYL). Here, we evaluated these SCRAs for their capacity to activate the human cannabinoid receptor 1 (CB1) via indirect measurement of G protein recruitment. Furthermore, we comparatively evaluated the results obtained from three in vitro assays, based on the recruitment of β‐arrestin 2 (βarr2 assay) or Gαi protein (mini‐Gαi assay), or binding of [35S]‐GTPγS. The observed efficacies (Emax) varied depending on the conducted assay. Statistical analysis suggests that the population means of the relative intrinsic activity (RAi) significantly differ for …
Total citations
2021202220232024412139